Methiothepin mesylate
Based on 2 publication(s) in Google Scholar
Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
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- Reinheit: 99.36%
- CAS. Nr.: 74611-28-2
- Formel: C21H28N2O3S3
- Molecular Weight:452.65
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Methiothepin mesylate
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Biologische Aktivität
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5-HT1A Receptor 7.10 (pKd) |
5-HT1A Receptor |
5-HT1B Receptor |
5-HT1C Receptor |
5-HT1D Receptor |
5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT5A Receptor |
5-HT5B Receptor |
5-HT6 Receptor |
5-HT7 Receptor |
5-HT1B Receptor 7.28 (pKd) |
5-HT1C Receptor 7.56 (pKd) |
5-HT1D Receptor 6.99 (pKd) |
5-HT5A Receptor 7.0 (pKd) |
5-HT5B Receptor 7.8 (pKd) |
5-HT6 Receptor 8.74 (pKd) |
5-HT7 Receptor 8.99 (pKd) |
5-HT2A Receptor 8.50 (pKi) |
5-HT2B Receptor 8.68 (pKi) |
5-HT2C Receptor 8.35 (pKi) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
56 nM
Compound: Methiothepin mesylate
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Antagonistic activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
Antagonistic activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
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[PMID: 27487565] |
| CHO-K1 | IC50 |
71 nM
Compound: Methiothepin mesylate
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Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
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[PMID: 27487565] |
Methiothepin mesylate is a 5-HT receptor antagonist, with pKds of 7.10, 7.28, 7.56, and 6.99 for 5-HT1A, 5HT1B, 5HT1C, 5HT1D[1]. Methiothepin mesylate also shows pKds of 7.0, 7.8, 8.74, and 8.99 for 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7, respectively[2]. Methiothepin exhibits high affinity at 5-HT2A, 5HT2B, and 5HT2C with pKis of 8.50, 8.68, and 8.35, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 74611-28-2
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Appearance Solid
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Molecular Weight 452.65
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Formel C21H28N2O3S3
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Color White to light yellow
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SMILES
CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(SC)C=C24)CC1.CS(=O)(O)=O
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Synonyms
Metitepine mesylate; Ro 8-6837 mesylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Insect Biochem Mol Biol
Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]2025 May:180:104312. PMID: 40245998 -
Gen Comp Endocrinol
Characterization of serotonin receptors Aj5-HTR2 and Aj5-HTR7 reveals potential roles in circadian regulation of Apostichopus japonicus. [Abstract]2026 Mar:379:114913. PMID: 41819218
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (552.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Schoeffter P, et al. 5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype. J Pharmacol Exp Ther. 1990 Jan;252(1):387-95. [Content Brief]
[2]. Knight AR, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. Epub 2004 Jul 30. [Content Brief]
[3]. Hoyer D, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev. 1994 Jun;46(2):157-203. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2092 mL | 11.0461 mL | 22.0921 mL | 55.2303 mL |
| 5 mM | 0.4418 mL | 2.2092 mL | 4.4184 mL | 11.0461 mL | |
| 10 mM | 0.2209 mL | 1.1046 mL | 2.2092 mL | 5.5230 mL | |
| 15 mM | 0.1473 mL | 0.7364 mL | 1.4728 mL | 3.6820 mL | |
| 20 mM | 0.1105 mL | 0.5523 mL | 1.1046 mL | 2.7615 mL | |
| 25 mM | 0.0884 mL | 0.4418 mL | 0.8837 mL | 2.2092 mL | |
| 30 mM | 0.0736 mL | 0.3682 mL | 0.7364 mL | 1.8410 mL | |
| 40 mM | 0.0552 mL | 0.2762 mL | 0.5523 mL | 1.3808 mL | |
| 50 mM | 0.0442 mL | 0.2209 mL | 0.4418 mL | 1.1046 mL | |
| 60 mM | 0.0368 mL | 0.1841 mL | 0.3682 mL | 0.9205 mL | |
| 80 mM | 0.0276 mL | 0.1381 mL | 0.2762 mL | 0.6904 mL | |
| 100 mM | 0.0221 mL | 0.1105 mL | 0.2209 mL | 0.5523 mL |
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